4-Phenyl-7-hydroxy-2-chinolon | 30034-41-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-Phenyl-7-hydroxy-2-chinolon
• 英文别名: 7-hydroxy-4-phenyl-2-quinolinone；7-hydroxy-4-phenylcarbostyril；7-hydroxy-4-phenyl-1H-quinolin-2-one；7-hydroxy-4-phenyl-1H-quinolin-2-one
• CAS: 30034-41-4
• 化学式: C₁₅H₁₁NO₂
• 分子量: 237.258
• InChiKey: LGSVELDCSDHDES-UHFFFAOYSA-N

物化性质

• 沸点：
  484.3±45.0 °C(Predicted)
• 密度：
  1.298±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-Phenyl-7-hydroxy-2-chinolon 在 potassium carbonate 、 potassium iodide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 26.0h， 生成 2,2-Dimethyl-8-phenyl-2,5-dihydro-1-oxa-5-aza-phenanthren-6-one
  参考文献：
  名称：

  Antitumor agents 1871: Synthesis and cytotoxicity of substituted 8,8-dimethyl-2H,8H-pyrano[6,5-h]quinoline-2-one and related compounds

  摘要：

  Several substituted 8,8-dimethyl-2H,8H-pyrano[6,5-h]quinoline-2-ones and related compounds were synthesized and evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines. The most active compound (3) showed significant cytotoxic activity with GI(50) values in the micromolar range. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00065-7
• 作为产物：
  描述：

  7-氨基-4-苯基-1H-喹啉-2-酮 在 硫酸 、 sodium nitrite 作用下， 以 水 为溶剂， 生成 4-Phenyl-7-hydroxy-2-chinolon
  参考文献：
  名称：

  简洁的区域特异性合成8,8-二甲基-2 H，8 H-吡喃并[6，5- h ]喹啉-2-酮及相关化合物

  摘要：

  描述了一种有效的方法，该方法通过克莱森重排进行8,8-二甲基-2 H，8 H-吡喃并[6,5 - h ]喹啉-2-酮和相关化合物的区域特异性合成。

  DOI：

  10.1016/s0040-4039(99)00821-7

文献信息

• [EN] QUINOLINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND USES THEREOF FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE QUINOLÉINE, LEURS PROCÉDÉS DE PRÉPARATION ET LEURS UTILISATIONS DANS LE TRAITEMENT DU CANCER
  申请人：LEAD DISCOVERY CENTER GMBH

  公开号：WO2020188049A1

  公开（公告）日：2020-09-24

  The present invention relates to compounds of the general formula (I): (I), wherein V, W, M, R, R and Y have the designations cited below, or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof, and to processes for the preparation of compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof. The invention also relates to compounds of the general formula(I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use as a medicament. Further, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use in the treatment of cancer. Moreover, the invention relates to compounds of the general formula(I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for treating cancer in simultaneous, alternating or subsequent combination with another cancer therapy.

  本发明涉及一般式（I）的化合物：（I），其中V、W、M、R、R和Y具有下文所述的符号，或其药学或兽医可接受的盐、水合物或溶剂化合物，以及制备一般式（I）的化合物或其药学或兽医可接受的盐、水合物或溶剂化合物的方法。该发明还涉及一般式（I）的化合物或其药学或兽医可接受的盐、水合物或溶剂化合物作为药物的用途。此外，该发明涉及一般式（I）的化合物或其药学或兽医可接受的盐、水合物或溶剂化合物用于癌症治疗的用途。此外，该发明涉及一般式（I）的化合物或其药学或兽医可接受的盐、水合物或溶剂化合物用于与另一种癌症治疗同时、交替或随后组合治疗癌症。
• Carbostyril derivatives, and antihistaminic agents containing the same
  申请人：Otsuka Pharmaceutical Co., Ltd.

  公开号：US04482560A1

  公开（公告）日：1984-11-13

  Novel carbostyril derivatives and their salts having antihistaminic effects and are useful as antihistaminic agents, represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a lower alkyl group which may have phenyl group(s) as the substituted group(s); R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), or a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups; R.sup.4 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; X is a halogen atom; Y is a lower alkylene group which may have hydroxyl group(s) as the substituent(s); n is 0, 1 or 2; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that when R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), then R.sup.4 should be neither a hydroxyl group nor a lower alkanoyl group.

  具有抗组胺效果并可用作抗组胺剂的新型碳基苯并噻唑衍生物及其盐，由通式（1）表示，其中R1为氢原子，较低的烯基基团，较低的炔基基团或较低的烷基基团，其可以具有苯基（作为取代基）;R2为氢原子，较低的烷基基团或苯基;R3为具有苯基（作为取代基）的较低烷基基团，或者是可以具有来自卤素原子，较低烷基基团和较低烷氧基的1至3个取代基的苯基;R4为氢原子，羟基或较低的烷酰基基团;X为卤素原子;Y为较低的烷基烯基基团，其可以具有氢氧基（作为取代基）;n为0，1或2;在碳基苯并噻唑骨架中3-和4-位置之间的碳-碳键为单键或双键;前提是当R3为具有苯基（作为取代基）的较低烷基基团时，R4不应为羟基或较低的烷酰基基团。
• QUINOLINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND USES THEREOF FOR THE TREATMENT OF CANCER
  申请人：Lead Discovery Center GmbH

  公开号：US20220169616A1

  公开（公告）日：2022-06-02

  The present invention relates to compounds of the general formula (I): (I), wherein V, W, M, R, R and Y have the designations cited below, or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof, and to processes for the preparation of compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof. The invention also relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use as a medicament. Further, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for use in the treatment of cancer. Moreover, the invention relates to compounds of the general formula (I) or a pharmaceutically or veterinary acceptable salt, hydrate or solvate thereof for treating cancer in simultaneous, alternating or subsequent combination with another cancer therapy.
• US4482560A
  申请人：——

  公开号：US4482560A

  公开（公告）日：1984-11-13
• US5410054A
  申请人：——

  公开号：US5410054A

  公开（公告）日：1995-04-25